| 摘要 |
<p>The invention comprises 17a -ethinyl-17b hydroxy - estra - b (10),9(11) - dien-3-one and a process for the preparation thereof by reacting 17a - ethynyl - 17b - hydroxy-estra-4,9(10)-dien3-one with a secondary amine so as to form the corresponding 3-enamino-17a -ethynyl-17b hydroxy - estra - 3,5(10),9(11) - triene of the formula: <FORM:0919434/IV (b)/1> (where R and R1 are alkyl groups, which may be the same or different, or together with the nitrogen atom constitute a heterocyclic ring containing nitrogen or both nitrogen and oxygen) and the latter is subjected to hydrolysis in an acid medium so as to yield the desired 17a -ethinyl-17b -hydroxy-estra-5(10), 9(11)-dien-3-one. As secondary amine there may be used pyrrolidine, piperidine or morpholine. Hydrolysis may be effected with formic or acetic acids.</p> |
